New compounds as telomerase inhibitors that fix the G-quadruplex structure of DNA or RNA, useful in the treatment of cancers

摘要

Compounds that fix the G-quadruplex structure of DNA or RNA are new. Compounds that fix the G-quadruplex structure of DNA or RNA and having the formula Ar1-(NR3)p-(CO)n-divider-(CO)m-(NR'3)q-Ar2 (I) are new. n, m, p, and q = 0 or 1; Ar1 = quinoline (optionally substituted by a group N(Ra)(Rb), or 1-4 C alkyl, or alkoxy), quaternized quinoline, benzamidine or pyridine; Ra, Rb = H or 1-4C alkyl; Ar2 = Ar1, a phenyl ring optionally substituted by halogen, alkoxy, CN, carbonyl amino optionally substituted by alkyl, guanyl, alkylthio, amino, alkylamino, dialkylamino, nitro, or alkyleneamino, an aromatic or non-aromatic mono-, bi- or tricyclic heterocycle having 0 - 2 heteroatoms per ring optionally substituted by alkyl, alkylene or alkenylene; R3, R'3 = H or alkyl; divider = triazine (optionally substituted by one or more halogens, alkyl, thio, oxy, or amino, themselves optionally substituted by alkyl), 5 or 6 membered heterocycle containing O, S, or N, phenyl, -NH-phenyl-NH-, NH-phenyl-CH2-NH-, -NH-CH2-phenyl-CH2-NH-, -NH-CH2-phenyl-NH-CH2-phenyl-CH2-, -CH2-phenyl, -phenyl-CH2-, -CH2-thienyl-, -thienyl-CH2-, -CH=CH-, or a diazine, all of these being optionally substituted. With the provisos that: (1) when the divider group is phenyl optionally substituted by CH2, n, m, p, and q = 1, and R3 and R'3 are H, then the nitrogen heterocycle and the aromatic ring are not both unsubstituted quinoline or quinoline substituted on the N atom by 1-6C alkyl; and (2) when the divider group is a triazine and p and q are both 1, then n and m are not both 0.